Design, synthesis and evaluation of malonic acid-based PTP1B inhibitors / 药学学报
Acta Pharmaceutica Sinica
;
(12): 367-373, 2012.
Artigo
em Chinês
| WPRIM
| ID: wpr-323034
ABSTRACT
Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. Phosphotyrosine (pTyr) is the substrate for PTP1B dephosphorylation. Malonic acid moiety was used herein as a mimic of the phosphate group in pTyr, and novel malonic acid derivatives 1-7 were designed, synthesized and evaluated as PTP1B inhibitors. Results from enzymatic assays indicated that compounds 3 and 4 exhibited potent inhibition against human recombinant PTP1B with IC50 values of 7.66 and 1.88 micromol x L(-1), respectively.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Relação Estrutura-Atividade
/
Desenho de Fármacos
/
Estrutura Molecular
/
Química
/
Concentração Inibidora 50
/
Inibidores Enzimáticos
/
Proteína Tirosina Fosfatase não Receptora Tipo 1
/
Malonatos
/
Metabolismo
Limite:
Humanos
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2012
Tipo de documento:
Artigo
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